Enzyme-Activatable Probe for Tumor Bimodal Imaging, Intraoperative Navigation, and Urinalysis

We develope an enzyme-activatable platform (NO₂-RGD-Gd) for the integrated urinary biomarker detection, highcontrast fluorescence-magnetic resonance (MR) dualmodal imaging, and real-time image-guided surgical navigation within a single molecule. The advantages, including the favorable tumor-targeting affinity (RGD peptide), high renal clearance efficiency, and tumor-specific fluorescence activation, are achieved by rationally engineering the molecular architecture. Benefiting from these characteristics, the NO₂-RGD-Gd effectively bridges the boundary between diagnosis and therapy, achieving outstanding combinatorial performance in in vivo applications. It allows early and precise diagnosis through urinary biomarkers, provides anatomical-pathological and molecular imaging information of tumor lesions via fluorescence-MR dual-modal imaging, and delineates tumor boundaries for accurate surgical navigation relying on tumor-targeted activatable fluorescence imaging signals. Furthermore, all these processes can be realized simply via intravenous injection, offering a more efficient and feasible strategy for integrated diagnostic and therapeutic applications.